沙丁胺醇在体外表现出雄激素活性。
Salbutamol exhibits androgenic activity in vitro.
作者信息
von Bueren André O, Ma Risheng, Schlumpf Margret, Lichtensteiger Walter
机构信息
Institute of Pharmacology and Toxicology, University of Zurich, Switzerland.
出版信息
Br J Sports Med. 2007 Dec;41(12):874-8; discussion 878. doi: 10.1136/bjsm.2007.035162. Epub 2007 May 17.
BACKGROUND
Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown.
AIM
To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro.
METHODS
The potential androgenic activity of salbutamol was investigated in vitro by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human mammary carcinoma cell line, MCF7-AR1.
RESULTS
The assay was validated with three known androgens; methyltrienolone (R1881), 5alpha-dihydrotestosterone (DHT) and danazol. IC50 values of R1881, DHT and danazol, 4.41x10(-11), 4.44x10(-11) and 1.08x10(-8) M, respectively, were in the ranges known from earlier studies. Our results demonstrate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93x10(-6) M. Anti-estrogenic or cytotoxic effects, which might have interfered with the assay, were excluded by additional experiments on wild-type MCF7 and MCF7-AR1 cells, respectively.
CONCLUSION
These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro.
背景
已表明沙丁胺醇静脉给药后可介导合成代谢作用。然而，沙丁胺醇合成代谢作用的机制仍不清楚。
目的
研究沙丁胺醇在体外介导合成代谢作用的潜在机制。
方法
通过A-Screen试验在体外研究沙丁胺醇的潜在雄激素活性，该试验测量雄激素受体（AR）阳性人乳腺癌细胞系MCF7-AR1增殖的雄激素依赖性抑制。
结果
该试验用三种已知雄激素进行验证；甲基三烯醇酮（R1881）、5α-二氢睾酮（DHT）和达那唑。R1881、DHT和达那唑的半数抑制浓度（IC50）值分别为4.41×10⁻¹¹、4.44×10⁻¹¹和1.08×10⁻⁸M，在早期研究已知范围内。我们的结果表明，沙丁胺醇具有雄激素活性，IC50值为8.93×10⁻⁶M。分别对野生型MCF7和MCF7-AR1细胞进行的额外实验排除了可能干扰该试验的抗雌激素或细胞毒性作用。
结论
这些数据表明，沙丁胺醇在体外通过雄激素受体激动活性发挥合成代谢作用。
Zotero 插件